Publications by authors named "Vija Gailite"
2-(3-(Naphthalen-2-yl)propanamido)cyclohex-1-enecarboxylic acid and its 6-hydroxynaphthalen-2-yl analogue are well-known hydroxyl-carboxylic acid (HCA) receptor HCA2 agonists. A series of novel aryl derivatives of 2-amidocyclohex-1-ene carboxylic acid that contained rigidity elements, such as an E-double bond, triple bond, and trans or cis-substituted cyclopropane rings, instead of the saturated ethane linker in the amide part of the molecules were designed and synthesized, and the derivatives' potency for the activation of HCA1, HCA2, and HCA3 receptors by 3'-5'-cyclic adenosine monophosphate (cAMP) assay were evaluated. The SAR studies revealed that the rigidifying of appropriate molecules enabled modulation of the potency and selectivity of the HCA2 receptor activation.
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- Enzymatic inhibition of histone deacetylase (HDAC) is a promising strategy for cancer treatment, leading to the development of new amide derivatives.
- Several of these compounds demonstrated strong HDAC inhibitory effects, with low IC(50) values in nanomolar ranges when tested on HeLa cells.
- The novel compounds, particularly one called (E)-N-[6-(hydroxyamino)-6-oxohexyl]-3-(7-quinolinyl)-2-propenamide, showed impressive results in vivo, significantly increasing the lifespan of mice with leukemia.